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/ Nilotinib/尼洛替尼

Nilotinib/尼洛替尼 {[allProObj[0].p_purity_real_show]}

货号：A448494 同义名： 尼罗替尼 (AMN-107) / AMN107

Nilotinib是一种口服可用的Bcr-Abl酪氨酸激酶抑制剂，具有抗肿瘤特性。

Nilotinib/尼洛替尼 化学结构 CAS号：641571-10-0
Nilotinib/尼洛替尼 化学结构
CAS号：641571-10-0
Nilotinib/尼洛替尼 3D分子结构
CAS号：641571-10-0
Nilotinib/尼洛替尼 化学结构 CAS号：641571-10-0
Nilotinib/尼洛替尼 3D分子结构 CAS号：641571-10-0
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Nilotinib/尼洛替尼 纯度/质量文件 产品仅供科研

货号：A448494 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
产品名称 Abl ↓ Bcr-Abl ↓ 其他靶点 纯度
NVP-BHG 712 +

c-Abl, IC50: 1.667 μM

 		99%+
KW-2449 +++

Abl, IC50: 14 nM

Abl (T315I), IC50: 4 nM

 		FLT3 99%+
Ponatinib ++++

Abl, IC50: 0.37 nM

 		98%
AT9283 99%+
Imatinib Mesylate +

v-Abl, IC50: 600 nM

 		c-Kit,PDGFR 99%
Danusertib ++

Abl, IC50: 25 nM

 		RET 99%+
Rebastinib ++++

u-Abl1 (T315I), IC50: 5 nM

p-Abl1 (native), IC50: 0.75 nM

 		FLT3,Tie-2 99%+
PP121 ++

Abl, IC50: 18 nM

 		VEGFR,PDGFR 99%+
GNF-7 +++

M351T, IC50: 133 nM

E255V, IC50: 122 nM

 		99%+
Olverembatinib dimesylate ++++

Abl, IC50: 0.34 nM

Abl (G250E), IC50: 0.35 nM

 		98%
Dasatinib monohydrate ++++

Abl , IC50: 0.6 nM

 		Src 98%
Dasatinib ++++

Abl, IC50: 0.6 nM

 		Src 98%
Bafetinib +++

Abl, IC50: 5.8 nM

 		98+%
GNF-2 +

Bcr-Abl (SUP-B15 cell line), IC50: 268 nM

Bcr-Abl (K562 cell line), IC50: 273 nM

 		98%+
Degrasyn +

Bcr-Abl, IC50: 1.8 μM

 		DUB/Deubiquitinase 99+%
GNF-5 ++

Bcr-Abl, IC50: 220 nM

 		99%
Radotinib ++

BCR-ABL1, IC50: 34 nM

 		98+%
PD173955 Src 99%+
Nilotinib ++

Bcr-Abl, IC50: <30 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 ALK1 ↓ ALK2 ↓ ALK3 ↓ ALK4 ↓ ALK6 ↓ Smad3 ↓ TGF-β ↓ TGFβRI/ALK5 ↓ TGFβRII ↓ 其他靶点 纯度
LDN193189 ++++

ALK1, IC50: 0.8 nM

 		++++

ALK2, IC50: 0.8 nM

 		+++

ALK3, IC50: 5.3 nM

 		+++

ALK6, IC50: 16.7 nM

 		99%+
LDN-212854 ++++

ALK1, IC50: 2.4 nM

 		++++

ALK2, IC50: 1.3 nM

 		+

ALK3, IC50: 85.8 nM

 		+

ALK4, IC50: 2133 nM

 		+

ALK5, IC50: 9276 nM

 		99%+
ML347 ++

ALK1, IC50: 46 nM

 		++

ALK2, IC50: 32 nM

 		98%
K02288 ++++

ALK1, IC50: 1.8 nM

 		++++

ALK2, IC50: 1.1 nM

 		++

ALK3, IC50: 34.4 nM

 		+++

ALK6, IC50: 6.4 nM

 		99%+
LDN-193189 2HCl ++++

ALK1, IC50: 0.8 nM

 		++++

ALK2, IC50: 0.8 nM

 		+++

ALK3, IC50: 5.3 nM

 		+++

ALK6, IC50: 16.7 nM

 		99%
LDN-214117 ++

ALK2, IC50: 24 nM

 		98%
DMH-1 +

ALK2, IC50: 107.9 nM

 		99%+
SB-505124 +

ALK4, IC50: 129 nM

 		++

ALK5, IC50: 47 nM

 		99%+
Vactosertib +++

ALK4, IC50: 13 nM

 		+++

ALK5, IC50: 11 nM

 		99%+
Alantolactone ✔ 98%
(E/Z)-SIS3 free base ✔ 97%
Pirfenidone ✔ 98%
Hesperetin ✔ 97%
RepSox ++++

TGFβR1(ALK5), IC50: 4 nM

 		98%
GW788388 +++

ALK5, IC50: 18 nM

 		98%
LY364947 ++

TGFβRI, IC50: 59 nM

 		+

TGFβRII, IC50: 0.4 μM

 		98%
SD-208 ++

TGF-βRI (ALK5), IC50: 48 nM

 		99%
SB-525334 +++

TGFβR1(ALK5), IC50: 14.3 nM

 		99%+
LY2109761 ++

TβRI, Ki: 38 nM

 		+

TβRII, Ki: 300 nM

 		99%+
Galunisertib ++

TβRI, IC50: 56 nM

 		98%
SB 431542 +

ALK5, IC50: 94 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Nilotinib/尼洛替尼 生物活性

靶点

  • Bcr-Abl

    Bcr-Abl, IC50:<30 nM
描述 The oncogenic tyrosine kinase Bcr-Abl plays a central role in the pathogenesis of chronic myelogenous leukemia, thus makes it as the therapy drug target. However, it is demonstrated that the mutations of Bcr-Abl kinase have been the most common mechanism of drug resistance, such as imatinib. Nilotinib is a potent and selective Bcr-Abl inhibitor with IC50 values of 15nM, as well as IC50 values ranging in 9-400nM for different Abl mutations except the T315l mutation (measured by in vitro kinase assays)[1]. Though Nilotinib was structured based on imatinib, in vitro study showed that Nilotinib showed differential sensitivity of Abl point mutations with imatinib[1][2]. Nilotinib inhibited proliferation of Ba/F3 cells expressing G250E, E255K(V), F317L, M351T, F486S, M244V, L248R, Q252H, Y253H, E255K, E279K, E282D, V289S, and L348M Bcr-Abl mutants at concentration<1μM, as well as tyrosine autophosphorylation of the E255K, E255V, F317L, M351T and F486S Bcr-Abl mutants with mean IC50 values of 150, 246, 41, 31 and 43 nM, respectively. Activity against PDGFR and c-Kit by Nilotinib also can be observed at concentration<200nM. Oral dose of 75mg/kg Nilotinib prolonged survival and decreased tumor burden in an imatinib-resistant Bcr-Abl mutant BMT model[2].
作用机制 Nilotinib was found to bind to the inactive conformation of Abl as observed for imatinib, resulting differential sensitivity of Abl point mutations by Nilotinib.[2]

Nilotinib/尼洛替尼 细胞实验

Cell Line
Concentration Treated Time Description References
HCT116 20 μM 24 h Nilotinib significantly enhanced MHC-I expression in HCT116 cells. J Transl Med. 2024 Aug 14;22(1):769.
SW480 10 μM 48 h Nilotinib significantly enhanced MHC-I expression in SW480 cells. J Transl Med. 2024 Aug 14;22(1):769.
TXL-2 cells 300 nM 21 days To evaluate the effect of nilotinib combined with AMD11070 on TXL-2 cells, the results showed that the combination treatment inhibited cell proliferation. Leukemia. 2011 Aug;25(8):1314-23.
Human valvular interstitial cells (VICs) 10 μM 24 h Nilotinib increased calcification and BMP-2 expression in VICs. Br J Pharmacol. 2022 Oct;179(19):4709-4721.
Human valvular interstitial cells (VICs) 10 μM 24 h Nilotinib significantly inhibited autophagic activity and decreased VIC viability. Br J Pharmacol. 2022 Oct;179(19):4709-4721.
Human Umbilical Vein Endothelial Cells (HUVEC) 0.01-20 µM 48 h Nilotinib inhibited the growth and viability of HUVEC, whereas Imatinib showed no comparable effects. Leukemia. 2017 Nov;31(11):2388-2397.
Human Coronary Artery Endothelial Cells (HCAEC) 0.01-20 µM 48 h Nilotinib inhibited the growth and viability of HCAEC, whereas Imatinib showed no comparable effects. Leukemia. 2017 Nov;31(11):2388-2397.
Human Microvascular Endothelial Cell Line (HMEC-1) 0.01-20 µM 48 h Nilotinib inhibited the growth and viability of HMEC-1, whereas Imatinib showed no comparable effects. Leukemia. 2017 Nov;31(11):2388-2397.
H295R cells 1, 5, 10 µM 72 h Nilotinib alone or in combination with mitotane induced more significant cell viability inhibition in monolayer and spheroid preparations. Cancer Cell Int. 2018 Mar 1;18:29.
ACC-T36 cells 10 µM 72 h Nilotinib alone or in combination with mitotane induced more significant cell viability inhibition in monolayer and spheroid preparations. Cancer Cell Int. 2018 Mar 1;18:29.
CD34+ hematopoietic stem cells 3.6 µM 15 days To study the effect of Nilotinib on NK cell differentiation, results showed that Nilotinib inhibited the recovery of CD56+ cells. Front Immunol. 2018 Oct 23;9:2433.

Nilotinib/尼洛替尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Bcr/Abl-positive ALL model Oral 75 mg/kg Once daily for 12 days To evaluate the effect of nilotinib combined with AMD11070 on the survival of Bcr/Abl-positive ALL mice, the results showed that the combination treatment significantly prolonged survival. Leukemia. 2011 Aug;25(8):1314-23.
Mice Hyperlipidemic mouse model Oral 30 mg/kg Once daily for 16 weeks Nilotinib significantly increased aortic valve thickness in mice. Br J Pharmacol. 2022 Oct;179(19):4709-4721.
Mice ApoE-/- mice Oral 2x37.5 mg/kg Twice daily for 8 weeks Nilotinib promoted atherosclerosis in ApoE-/- mice, whereas Imatinib showed no comparable effects. Leukemia. 2017 Nov;31(11):2388-2397.
Mice BC CML mouse model Oral gavage 30 mg/kg Once daily for 3 weeks To evaluate the therapeutic effect of Nilotinib alone or in combination with M-miR-142 and PD-1 antibody in BC CML mouse models. The results showed that Nilotinib alone significantly reduced leukemic burden and prolonged survival, while the combination with M-miR-142 and PD-1 antibody ("triplet" therapy) further reduced leukemic burden and significantly extended survival. Nat Commun. 2025 Feb 1;16(1):1253
Mice MC38 and CT26 tumor models Oral 25 mg/kg Daily The combination of nilotinib with anti-PDL1 antibody significantly inhibited tumor growth and enhanced CD8+ T cell cytotoxicity. J Transl Med. 2024 Aug 14;22(1):769.

Nilotinib/尼洛替尼 动物研究

Dose Rat: 5 mg/kg - 40 mg/kg[3] (p.o.) Mice: 30 mg/kg - 300 mg/kg[3] (p.o.), 10 mg/kg[4] (i.p.)
Administration p.o., i.p.

Nilotinib/尼洛替尼 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00785785 - Completed - -
NCT01220648 Chronic Myeloid Leukemia Phase 1 Completed - Germany ... 展开 >> Novartis Investigative Site Leipzig, Germany, 04103 收起 <<
NCT01806571 Untreated Adult Acute Myeloid ... 展开 >>Leukemia 收起 << Phase 2 Active, not recruiting April 18, 2020 United States, Arizona ... 展开 >> Mayo Clinic in Arizona Scottsdale, Arizona, United States, 85259 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 收起 <<

Nilotinib/尼洛替尼 参考文献

[1]O'Hare T, Walters DK, et al. In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res. 2005 Jun 1;65(11):4500-5.

[2]Weisberg E, Manley PW, et al. Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. Cancer Cell. 2005 Feb;7(2):129-41.

Nilotinib/尼洛替尼 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.44mL

1.89mL

0.94mL

18.89mL

3.78mL

1.89mL

Nilotinib/尼洛替尼 技术信息

CAS号641571-10-0
分子式C28H22F3N7O
分子量 529.52
SMILES Code O=C(NC1=CC(C(F)(F)F)=CC(N2C=C(C)N=C2)=C1)C3=CC=C(C)C(NC4=NC=CC(C5=CC=CN=C5)=N4)=C3
MDL No. MFCD09833716
别名 尼罗替尼 (AMN-107) ;AMN107
运输蓝冰
InChI Key HHZIURLSWUIHRB-UHFFFAOYSA-N
Pubchem ID 644241
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 12 mg/mL(22.66 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Nilotinib | AMN107 | 尼罗替尼 (AMN-107) | Bcr-Abl | TGF-beta/Smad | AmBeed-信号通路专用抑制剂 | Nilotinib/尼洛替尼 纯度/质量文件 | Nilotinib/尼洛替尼 亚型比较 | Nilotinib/尼洛替尼 生物活性 | Nilotinib/尼洛替尼 动物研究 | Nilotinib/尼洛替尼 临床数据 | Nilotinib/尼洛替尼 参考文献 | Nilotinib/尼洛替尼 实验方案 | Nilotinib/尼洛替尼 技术信息

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